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Compound Detail

CHEMBL1641687

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Cl.Clc1ccc2c(N=C3NCCN3)n[nH]c2c1

Basic Information

ChEMBL ID CHEMBL1641687
Phase Preclinical
Structure Type MOL
InChI Key GPHZBMUZIYLGFW-UHFFFAOYSA-N
Parent Compound CHEMBL1739205
Active Moiety CHEMBL1739205
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

235.7
MW (Da)
1.40
ALogP
2
HBA
3
HBD
65.1
PSA (Ų)
0.70
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H11Cl2N5
MW 272.14
Aromatic Rings 2
Heavy Atoms 16
NP-Likeness -1.11

Activity Summary

Ki 3 meas. best 6.41
IC50 1 meas. best 5.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 6.41 6.41 386.0 1
Nischarin
CHEMBL5221
Ki 6.39 6.39 410.0 1
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 6.3 6.3 502.0 1
Nischarin
CHEMBL5221
IC50 5.7 5.7 2010.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21129985 10.1016/j.bmc.2010.11.020 Nischarin 2
21129985 10.1016/j.bmc.2010.11.020 Adrenergic receptor alpha-1 1
21129985 10.1016/j.bmc.2010.11.020 Adrenergic receptor alpha-2 1
21129985 10.1016/j.bmc.2010.11.020 Unchecked 1

Data from ChEMBL 36 via Core Engine